Prokinetics influence the pharmacokinetics of rabeprazole.
BACKGROUND
Proton pump inhibitors (PPIs) are unstable at a low PH. Accelerated transfer of PPIs to the upper small intestine may influence the pharmacokinetics of PPIs.


OBJECTIVE
To see if concomitant use of mosapride citrate with rabeprazole sodium influences the pharmacokinetics of the PPI.


METHODS
Two-way crossover pharmacokinetic studies were conducted in 9 healthy subjects. 20 mg of rabeprazole was given orally and plasma was obtained before and 1, 2, 3, 4, 5, 6 and 8 h after the dosing. Two weeks later, 5 mg of mosapride was given concomitantly with rabeprazole and plasma was collected as above. The plasma concentrations of rabeprazole were determined by high-performance liquid chromatography. The maximum plasma concentrations (C(max)) and the area under the time-plasma concentration curve (AUC) of rabeprazole, and the time to maximum plasma concentration (t(max)) were compared in the presence or absence of mosapride.


RESULTS
Concomitant use of mosapride resulted in significant increases of mean C(max) and mean AUC with ratios of 1.57 and 1.47, respectively. The median t(max) changed from 4 to 3 h, although the change was not significant.


CONCLUSIONS
Mosapride significantly influenced pharmacokinetics of rabeprazole. Co-administration of mosapride could have some favorable effect in PPIs-based therapy.
Arai
Katsuhito
K
Department of Gastroenterology, Showa University School of Medicine, Hatanodai, Shinagawaku, Tokyo, Japan.
Takeuchi
Yoshiaki
Y
Watanabe
Hideki
H
Tsukurimichi
Atsushi
A
Uchida
Naoki
N
Imawari
Michio
M
D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000097:blood* / Q000493:pharmacokinetics*; D000328:Adult; D019540:Area Under Curve; D001549:Benzamides / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004359:Drug Therapy, Combination; D004791:Enzyme Inhibitors / Q000097:blood* / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D009025:Morpholines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D064750:Rabeprazole
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D001549:Benzamides; D004791:Enzyme Inhibitors; D009025:Morpholines; D064750:Rabeprazole; C062720:mosapride